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Ro 41-5253
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Ro 41-5253图片
CAS NO:144092-31-9
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品介绍
Ro 41-5253 是一种具有口服活性的选择性维甲酸受体RARα拮抗剂。Ro 41-5253 可以与 RARα 结合而不诱导转录或影响 RAR/RXR 异二聚化和 DNA 结合。Ro 415253 可抑制癌细胞增殖并诱导细胞凋亡 (apoptosis),具有抗肿瘤活性。
生物活性

Ro 41-5253 is an orally active selective retinoic acid receptor alpha (RARα) antagonist. Ro 41-5253 can bind RARα without inducing transcription or affectingRAR/RXRheterodimerization and DNA binding. Ro 41-5253 can inhibitcancercell proliferation and induceapoptosis, has antitumor activity[1][2].

IC50& Target

IC50: 60 nM (RARα), 2.4 μM (RARβ), 3.3 μM (RARγ)[3].

体外研究
(In Vitro)

Ro 41-5253 (1 nM-10 μM, 10 days) significantly inhibits MCF-7 and ZR 75.1 cell proliferation and induces cell apoptosis in a time and dose-dependent manner[1].

Cell Proliferation Assay[1]

Cell Line:Human breast-carcinoma lines MCF-7 and ZR 75.1
Concentration:1 nM-10 μM
Incubation Time:10 days
Result:Inhibited 81% MCF-7 cell growth at 10 μM, 30% cell growth at 1 μM and no significant inhibitory effect at concentrations below 0.1 μM.
Inhibited 74% ZR 75.1 cell growth at 10 μM, 63% cell growth at 1 μM and 42% cell growth at 0.1 μM.

Apoptosis Analysis[1]

Cell Line:Human breast-carcinoma lines MCF-7 and ZR 75.1
Concentration:1 nM-10 μM
Incubation Time:10 days
Result:Induced 28.5, 21.6, 16 and 12% of MCF-7 cells apoptosis at 10 μM, 1 μM, 0.1 μM and 0.01 μM respectively on the fourth day while induced 58, 51, 36 and 21% of cells apoptosis at 10 μM, 1 μM, 0.1 μM and 0.01 μM respectively after six days.
Induced 80, 65, 43 and 29% of ZR 75.1 cells apoptosis at 10 μM, 1 μM, 0.1 μM and 0.01 μM respectively on the sixth day.
体内研究
(In Vivo)

Ro 41-5253 (oral gavage, 10-600 mg/kg, once a week, 4 weeks) can reduce tumor volume in female athymic Balb/mice transplanted with MCF-7 cell line[2].

Animal Model:Six-week-old female athymic Balb/mice transplanted with MCF-7 cell line[2]
Dosage:10, 30, 100, 300 and 600 mg/kg
Administration:Oral gavage; once a week; 4 weeks
Result:Resulted in a reduction in tumor volume at doses of 10, 30 and 100 mg/kg with no toxic side effects.
分子量

484.65

性状

Solid

Formula

C28H36O5S

CAS 号

144092-31-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL(206.33 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.0633 mL10.3167 mL20.6334 mL
5 mM0.4127 mL2.0633 mL4.1267 mL
10 mM0.2063 mL1.0317 mL2.0633 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.16 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.16 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。